Table 4.
Compound | mean A->B Papp (×10-6cm s-1) | Test species | Mean remaining parent, with NADPH (%) | Mean remaining parent, free of NADPH (%) |
---|---|---|---|---|
2 | 18.7 | Human | 96.8 | 84.8 |
Mouse | 79.4 | 110 | ||
19 | 16.5 | Human | 90.7 | 106 |
Mouse | 77.6 | 102 | ||
Verapamile | Human | 8.4 | 89.4 | |
Mouse | 6.0 | 96.5 | ||
Warfarin | 25.3 | Human | 102 | 96.7 |
Mouse | 104 | 101 | ||
Ranitidine | 0.24 |
Papp: Caco 2 apparent permeability. Permeability ranking: Low: <0.5; Moderate: 0.5 - 5; High: > 5. For permeability measurements 10 μM concentration was used and 2 h assay time. For metabolic stability, 1 μM concentration and 0 and 60 min incubation time was used. Test species represent either human or mouse microsomes.